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Compound Detail

CHEMBL2112905

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COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL2112905
Phase Preclinical
Structure Type MOL
InChI Key CRCRPVGVFIWNEN-UHFFFAOYSA-N
Parent Compound CHEMBL2219567
Active Moiety CHEMBL2219567
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

354.4
MW (Da)
1.95
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.86
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H28Cl2N4O2
MW 427.38
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -2.03

Activity Summary

Ki 3 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 7.62 7.62 23.9 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.23 7.23 58.6 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12477356 10.1021/jm020952a D(3) dopamine receptor 2
12477356 10.1021/jm020952a D(2) dopamine receptor 2
12477356 10.1021/jm020952a D(4) dopamine receptor 1
12477356 10.1021/jm020952a 5-hydroxytryptamine receptor 1A 1
12477356 10.1021/jm020952a Adrenergic receptor alpha-1 1
12477356 10.1021/jm020952a No relevant target 1

Data from ChEMBL 36 via Core Engine